کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1372073 981865 2010 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Polar 3-alkylidene-5-pivaloyloxymethyl-5′-hydroxymethyl-γ-lactones as protein kinase C ligands and antitumor agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Polar 3-alkylidene-5-pivaloyloxymethyl-5′-hydroxymethyl-γ-lactones as protein kinase C ligands and antitumor agents
چکیده انگلیسی

A series of DAG-lactones with polar 3-alkylidene substituents have been investigated as PKC-α ligands and antitumor agents. Extensive analysis of structure–activity relationships for the 3-alkylidene chain revealed that polar groups such as ether, hydroxyl, aldehyde, ester, acyloxy, and amido were tolerated with similar binding affinities and reduced lipophilicities compared to the corresponding unsubstituted alkylidene chain. Among the derivatives, compounds 5, 6 and 8 with an ether type of side chain showed high binding affinities in range of Ki= 3–5 nM and excellent antitumor profiles, particularly against the colo205 colon cancer and the K562 leukemia cell lines.

DAG-lactones 5, 6 and 8 with an ether type of side chain showed high binding affinities in range of Ki = 3–5 nM and excellent antitumor profiles.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 3, 1 February 2010, Pages 1008–1012
نویسندگان
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